This invention relates to the unique combination of three novel dietary supplements for use in a weight loss program.
The worldwide phenomenon of weight gain, despite various attempts at dietary intervention and exercise, indicates that the current mechanisms of regulating energy balance and body weight are not able to cope with obesity-promoting genetic makeup as well as the modern food environment, where calories are abundant and relatively inexpensive.
Moderate weight loss achievements, however, are recognised to have major health benefits for overweight individuals, and increases life-expectancy in those with obesity-related complications. A reduced energy intake combined with increased energy expenditure is known to be an effective weight-loss strategy. Research however has documented that only one third of those trying to lose weight reported eating fewer calories and exercising more. In addition, it has been estimated that 90% of those who lose weight through dieting will return to their original weight within 2-5 years.
This suggests that mono-therapy to reduce body weight cannot cope with the level of over-consumption triggered by modern society. It has therefore been proposed that combination therapies might provide a better future solution.
Rather than the current single-product/single-programme approach to treat obesity, this invention relates to a usage in combination of three novel nutritional agents simultaneously, with each agent targeting a different obesity-promoting category.
Used on their own, each of the three nutritional agents displays a unique weight-loss benefit within its own distinctive category and can effectively be used to treat or prevent obesity as a single or standalone treatment strategy.
This patent application, however, is based on the strategy that the combination of the three agents simultaneously is novel, synergistic and unique, and presents an improvement to prior models. This postulation is supported by original research that demonstrates that the combination of the three products simultaneously, achieves better results, compared to each agent used as a standalone agent during testing.
Numerous mechanisms control appetite, behaviour and energy regulation. For clarification purposes, these factors will be divided into three broad categories, namely: A—behaviour B—metabolism and C—food environment, and will be discussed in this sequence in this specification.
Category A: Behaviour
Most people gain weight because they eat too much. This could merely be because of bad habits, but often over-eating stems from emotional and medical conditions that make appetite control very difficult. The inventor has demonstrated that large numbers of obese individuals had undiagnosed psychological disorders such as the Binge Eating Disorder (Obsessive Compulsive Disorder), Attention Deficit Disorder (ADHD/ADD) and other mood disorders, (such as depression) and anxiety disorders (such as Generalised Anxiety Disorder), conditions that all lower levels of compliance and motivation. Giving these individuals a meal-plan of whatever kind without helping them address their underlying perceptive emotional disorder sets them up for failure right from the start and is therefore a futile exercise.
Successful weight-loss requires sustained effort, fuelled by motivation, which in turn is dependent on many other factors, including mood. Happiness and contentment are not static processes and it is difficult to maintain positive emotions like optimism, self-confidence and emotional tranquillity. Many persons must deal with difficult people on a daily basis, and can become emotionally drained and physically exhausted by numerous responsibilities. A successful solution to this problem has led the inventor to develop a mood stabiliser.
Category B: Metabolism
The phenomenon where some individuals can consume significantly more food calories than others, without gaining weight, is well known. This has been attributed to differences, some genetic and others acquired, which are numerous and complex, but can in many instances be explained on the basis of an acquired medical condition called ‘insulin resistance’, of which obesity is a major precipitating factor.
The single most important controller of organic metabolism is the hormone insulin, and not the thyroid hormone, as what is often mistakenly stated.
Insulin has several different effects that lead to fat accumulation in adipose tissue. Firstly, insulin promotes fat synthesis. When the quantity of glucose that enters the liver cells is more than what can be stored as glycogen, insulin promotes the conversion of excess glucose into fatty acids. These fatty acids are subsequently packaged as triglycerides in very low density lipoproteins and transported to the adipose tissue where they are deposited as fat. However, insulin also increases the utilisation of glucose by most of the body's tissues, which automatically decreases the utilisation of fat, thus functioning as a “fat sparer”.
Secondly, insulin plays a role in fat storage. By inhibiting the action of hormone-sensitive lipase, an enzyme that causes hydrolysis of the triglycerides already stored in the fat cells, insulin inhibits the release of fatty acids into the circulating blood stream, thereby promoting obesity. Insulin also promotes glucose transport through the cell membrane into the fat cells in the same way that it promotes glucose transport into the musde cells. Although some of this glucose is then utilized to synthesize small amounts of fatty acids, the glucose also forms large quantities of glycerophosphate which supplies the glycerol backbone that combines with fatty acids to form triglycerides molecules which are a dominant storage form of fat in adipose cells. Therefore, when insulin is not available, storage of a large amount of fatty acids transported from the liver via lipoproteins is almost totally blocked.
Various studies have investigated the role that insulin plays in weight gain. In the United Kingdom Prospective Diabetes Study (UKPDS), for example, increased weight gain was directly related to improved glycaemic control and intensification of therapy with all pharmacotherapies, (with the exception of the diabetic drug metformin). However, weight gain was greatest in a group treated with insulin, where patients gained on average 6.5 kg. In addition, data from the Diabetes Control and Complication Trial (DCCT) demonstrated that insulin-associated weight gain was significantly greater in patients receiving intensified insulin intervention, compared to conventional intervention.
Fat cells have historically been accredited with two main functions, namely that of storing energy and preserving body temperature via insulation. In the presence of excess intra-abdominal (visceral) fat, however, fat cells, once filled with fat, also assume a hormonal function by manufacturing and releasing various chemical substances called inflammatory cytokines, able to mimic or interfere with normal hormonal functions. For reasons not completely understood, some of these inflammatory cytokines disrupt insulin's role on cellular level (at the insulin receptor that regulates the glucose portal across the cell membrane) and render insulin less effective. The medical term for this condition is ‘insulin resistance’. To get the same task done as before, the body compensates by producing even more insulin, and insulin levels rise above the norm.
Because of insulin's obesity-promoting effects, insulin resistance makes one more prone to gaining weight than before. In addition, it also makes it more difficult for one to lose weight. Once this condition sets in, a vicious cycle begins, explaining why many obese individuals, once burdened with excess visceral fat, experience that their metabolism has effectively slowed down.
The invention in this category is based on the proposition that aspects of fat breakdown and use for providing energy are enhanced in the absence of insulin. This can occur normally between meals when secretion of insulin is minimal but the effect becomes extreme in diabetes mellitus when secretion of insulin, is almost absent. When this happens, the aforementioned effects of insulin causing the production and storage of fat, are reversed. A dominant effect is that the enzyme hormone-sensitive lipase in the fat cells becomes strongly activated. This causes hydrolysis of stored triglycerides, releasing large quantities of fatty acids and glycerol from the adipose tissue into the circulating blood. The net effect is significant weight-loss.
A goal in this respect is a strategy in which the insulin level is lowered to a value which is still healthy but which does not promote fat deposition and fat storage, thereby counteracting insulin's obesity-promoting effects.
The invention is inter alia based on the use of a combination of naturally derived compounds and plant extracts that display complementary and synergistic pharmaceutical effects, all of which have been proven to be useful for the treatment or alleviation of insulin resistance. The mode of action is via an unique mechanism, which optimises catabolic metabolism by lowering insulin levels and increasing the usage of fat for energy purposes, thereby assisting with weight loss.
Category C: The Food Environment
Our caveman forefathers used considerable amounts of energy and covered great distances on foot in search of food. Their meals, consisting mainly of low energy-dense foods, were often infrequent and interrupted by regular periods of famine. They also utilized large amounts of energy to maintain their body heat, especially in colder climates and in meagre habitats. In order to survive periods of starvation, the caveman's body perfected ways to store excess energy in the form of body fat. Those with more efficient storage systems had a significant advantage over their less padded friends during periods of famine.
Besides the caveman's body developing more efficient storage systems, the caveman's mind was also gearing for survival, and evolved to prevent weight loss at all costs. This basic instinct comes from the dinosaurs, inherited by cavemen (Homo erectus) and passed along to humans (Homo sapiens). If excess calories are available, appetite promotes weight gain by ensuring that the individual rather eats “too much” than “too little”. Matching energy intake and energy expenditure is extremely difficult. A small mismatch of, for example, 1% can lead to the accumulation of 10 000 calories per year, resulting in a weight gain of 1-2 kg per annum.
Modern day man, unlike cavemen, does not experience periods of famine, but still has the same ability to store energy very efficiently. The paradigm has however changed considerably and current lifestyles are vastly different. Food, now significantly more energy-dense for cavemen, has become abundant and many modern lives and social activities revolve around eating. Whilst genetics may permit the problem to occur, the food environment in the form of energy-rich food that is freely available at fast-food restaurants that line our roadways, and the rows of candies at checkout counters drive it.
The worldwide phenomenon of weight gain therefore indicates that the current mechanisms of regulating energy balance are clearly not able to cope with the prevailing obesity-promoting environment. Various mechanisms control appetite and energy intake and much attention has been focused upon the development of anti-obesity drugs that act on the central nervous system and reduce appetite. The withdrawal of numerous central working appetite suppressant drugs, however, such as fenfluramine, rimonabant and sibutramine (in Europe and under consideration in the US), suggest that targeting this pathway is not without problems.
Alternative options are agents that act on the periphery, namely the gastro-intestinal system, to block or prevent calorie absorption. The fat blocker orlistat, marketed under the trade name Xenical and Alli, falls into this category and is currently the only drug registered for the treatment of obesity in Europe.
It is well known that diets high in fat lead to weight gain because of energy overconsumption. This is mainly due to fat's high energy content and low potential for producing satiety. On the other hand, the excess consumption of refined carbohydrates found in sweet snack foods, sodas and desserts is also a major cause for weight gain. Fat, like refined carbohydrates, is rarely eaten in isolation, but more likely in combination. Good examples are French fries and ice cream.
Fat contains more than twice the amount of energy as the same quality of carbohydrate and protein. The human intestine is able to absorb 95% of all dietary fat, and it is therefore not surprising that a high fat diet is readily converted into fatty tissue, especially in individuals with a slow metabolic rate.
In the typical Western diet the dominant source (90%) of fat comes packaged as triglycerides. Each triglyceride consist of three smaller building blocks, called fatty acids, bonded together by a larger carrier molecule called glycerol. Triglyceride molecules are far too large to be absorbed through the intestinal wall, and therefore need to be broken down into smaller particles. This happens during the process of digestion, when fat-digesting enzymes split the bonds between fatty acids and set them free. Once released, each individual fatty acid freely passes through the wall of the small intestine and enters the body.
Fats are medically called ‘lipids’. Fat digestion is therefore called ‘lipolysis’ and the fat-digesting enzymes responsible for this process are the ‘lipases”. There are several different lipases, released throughout the gastro-intestinal tract. Lipolysis takes place via the combined action of different lipases. The rate at which lipolysis takes place and the consequent supply of free fatty acids to the body can be affected by various factors. These include certain biochemical agents, many of which are naturally occurring or derived from nature.
Like triglycerides, most carbohydrates are too large to be absorbed into the system without the splicing action of digestive enzymes. All carbohydrates are constructed from the elements carbon, hydrogen and oxygen, arranged in a three dimensional ring-like structure. A single ring is called a monosaccharide, two rings are a disaccharide, whilst those with more than two rings are the polysaccharides. For obvious reasons, monosaccharides are the smallest carbohydrate molecules and can be absorbed directly into the body without the need for digestion. Monosaccharides include glucose, the dominant energy molecule of the body, as well as fructose or ‘fruit sugar’, naturally found in fruit and fruit juice.
The disaccharides include table sugar and milk sugar, whilst the polysaccharides form the various starches. These two groups are the most important source of calories consumed in the average Western diet. Being too large to be absorbed, both disaccharides and polysaccharides require reduction through digestion into smaller molecules like glucose and fructose which can be absorbed and utilised as energy.
Like fat, the digestion of carbohydrate begins in the mouth and continues in the small intestines by the action of various digestive enzymes, mostly produced by the pancreas. This process is completed by another group of enzymes found in the intestines, which include maltase, sucrase, and lactase, collectively known as the aplha-glucosidases.
Nutrients are essential to health and the dominant reason all living creatures must eat a variety of nutritious food. Nutrients enter the body and are absorbed via the intestines. Antinutrients, however, are agents that block or interfere with the absorption of nutrients. Antinutrients are either natural or synthetic compounds and are found at some level in almost all foods for a variety of reasons, including food items that we consume on a daily basis. A common example is phytic acid, found abundantly in sodas and junk food. Phytic acid has the ability to form insoluble complexes with calcium, zinc, iron and copper, thereby reducing their absorption in the intestines and potentially causing a shortage.
Numerous antinutrients are also known to inhibit the action of digestive enzymes, including the lipases and alpha-glucosidases. In this field the inventor based his research and developed a novel unique product which is able to block carbohydrate and fat digestion simultaneously, thereby blocking the absorption of calories from both these sources after consumption.